HRP20221385T1 - Macrocyclic compound and uses thereof - Google Patents

Macrocyclic compound and uses thereof Download PDF

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Publication number
HRP20221385T1
HRP20221385T1 HRP20221385TT HRP20221385T HRP20221385T1 HR P20221385 T1 HRP20221385 T1 HR P20221385T1 HR P20221385T T HRP20221385T T HR P20221385TT HR P20221385 T HRP20221385 T HR P20221385T HR P20221385 T1 HRP20221385 T1 HR P20221385T1
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cancer
compound
use according
pharmaceutically acceptable
her2
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HRP20221385TT
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Croatian (hr)
Inventor
Yoshito Kishi
Kazunobu Kira
Ken Ito
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President And Fellows Of Harvard College
Eisai R&D Management Co., Ltd.
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Priority claimed from US15/814,105 external-priority patent/US9938288B1/en
Application filed by President And Fellows Of Harvard College, Eisai R&D Management Co., Ltd. filed Critical President And Fellows Of Harvard College
Publication of HRP20221385T1 publication Critical patent/HRP20221385T1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/22—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/04—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Saccharide Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Display Devices Of Pinball Game Machines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Claims (15)

1. Spoj sljedeće strukture: [image] ili njegova farmaceutski prihvatljiva sol.1. Compound of the following structure: [image] or a pharmaceutically acceptable salt thereof. 2. Farmaceutski pripravak naznačen time što sadrži spoj prema zahtjevu 1, ili njegovu farmaceutski prihvatljivu sol, u farmaceutski prihvatljivom nosaču.2. Pharmaceutical preparation characterized in that it contains the compound according to claim 1, or its pharmaceutically acceptable salt, in a pharmaceutically acceptable carrier. 3. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1 za uporabu u inhibiciji rasta tumora ili raka naznačenog time što ima angiogenezu, invaziju ili metastazu.3. A compound or a pharmaceutically acceptable salt thereof according to claim 1 for use in inhibiting the growth of a tumor or cancer characterized by angiogenesis, invasion or metastasis. 4. Spoj ili njegova farmaceutski prihvatljiva sol prema zahtjevu 1 za uporabu u liječenju tumora ili raka naznačenog time što ima angiogenezu, invaziju ili metastazu.4. A compound or a pharmaceutically acceptable salt thereof according to claim 1 for use in the treatment of a tumor or cancer characterized by angiogenesis, invasion or metastasis. 5. Spoj za uporabu prema zahtjevu 3 ili 4, naznačen time što je rak, rak glave i vrata, rak dojke, rak jednjaka, rak maternice, rak jajnika, kolorektalni rak, rak endometrija, rak želuca, rak tankog crijeva, rak mokraćnog mjehura ili sarkom.5. Compound for use according to claim 3 or 4, characterized in that it is cancer, head and neck cancer, breast cancer, esophageal cancer, uterine cancer, ovarian cancer, colorectal cancer, endometrial cancer, stomach cancer, small bowel cancer, bladder cancer or sarcoma. 6. Spoj za uporabu prema zahtjevu 5, naznačen time što je rak: (a) rak glave i vrata, poželjno pri čemu je rak karcinom pločastih stanica glave i vrata (SCCHN) ili adenoidni cistični karcinom; ili (b) rak dojke, poželjno pri čemu je rak dojke (i) HER2-pozitivan rak dojke, ili (ii) HER2-negativan rak dojke, ili (iii) trostruko negativan rak dojke; ili (c) kolorektalni karcinom; ili (d) rak jednjaka, poželjno pri čemu je rak jednjaka adenokarcinom jednjaka; ili (e) rak maternice; ili (f) rak jajnika; ili (g) sarkom, poželjno pri čemu je sarkom, sarkom maternice, fibrosarkom, sinovijalni sarkom, sarkom mekog tkiva ili angiosarkom; ili (h) rak želuca; ili (i) rak tankog crijeva, poželjno pri čemu je rak tankog crijeva adenokarcinom tankog crijeva; ili (j) rak mokraćnog mjehura; ili (k) urotelni karcinom.6. Compound for use according to claim 5, characterized in that cancer: (a) head and neck cancer, preferably wherein the cancer is squamous cell carcinoma of the head and neck (SCCHN) or adenoid cystic carcinoma; or (b) breast cancer, preferably wherein the breast cancer is (i) HER2-positive breast cancer, or (ii) HER2-negative breast cancer, or (iii) triple-negative breast cancer; or (c) colorectal cancer; or (d) esophageal cancer, preferably wherein the esophageal cancer is esophageal adenocarcinoma; or (e) uterine cancer; or (f) ovarian cancer; or (g) sarcoma, preferably a sarcoma, uterine sarcoma, fibrosarcoma, synovial sarcoma, soft tissue sarcoma or angiosarcoma; or (h) stomach cancer; or (i) small bowel cancer, preferably wherein the small bowel cancer is small bowel adenocarcinoma; or (j) bladder cancer; or (k) urothelial carcinoma. 7. Spoj za uporabu prema bilo kojem od zahtjeva 4-6, za uporabu u kombinaciji s protutijelom proteina programirane smrti (PD-1).7. A compound for use according to any one of claims 4-6, for use in combination with a programmed death protein (PD-1) antibody. 8. Spoj za uporabu prema bilo kojem od zahtjeva 4-6, za uporabu u kombinaciji s protutijelom L1 proteina programirane smrti (PD-L1).8. A compound for use according to any one of claims 4-6, for use in combination with an antibody to programmed death protein L1 (PD-L1). 9. Spoj za uporabu prema bilo kojem od zahtjeva 4-6, za uporabu u kombinaciji s anti-EGFR (receptor epidermalnog faktora rasta) protutijelom, poželjno pri čemu je anti-EGFR protutijelo anti-EGFR mAb, i/ili rak je rak glave i vrata, poželjno pri čemu je rak karcinom pločastih stanica glave i vrata (SCCHN), i/ili anti-EGFR mAb je cetuksimab.9. A compound for use according to any one of claims 4-6, for use in combination with an anti-EGFR (epidermal growth factor receptor) antibody, preferably wherein the anti-EGFR antibody is an anti-EGFR mAb, and/or the cancer is head cancer and neck, preferably wherein the cancer is squamous cell carcinoma of the head and neck (SCCHN), and/or the anti-EGFR mAb is cetuximab. 10. Spoj za uporabu prema bilo kojem od zahtjeva 4-6, za uporabu u kombinaciji s HER2 protutijelom (receptor humanog epidermalnog faktora rasta), poželjno pri čemu je HER2 protutijelo HER2 mAb, i/ili rak je rak dojke, i/ili HER2 mAb je trastuzumab.10. A compound for use according to any one of claims 4-6, for use in combination with a HER2 antibody (human epidermal growth factor receptor), preferably wherein the HER2 antibody is a HER2 mAb, and/or the cancer is breast cancer, and/or HER2 The mAb is trastuzumab. 11. Spoj za uporabu prema bilo kojem od zahtjeva 4-10 kod subjekta, pri čemu je spoj ili njegova farmaceutski prihvatljiva sol u farmaceutski prihvatljivom nosaču.11. A compound for use according to any one of claims 4-10 in a subject, wherein the compound or a pharmaceutically acceptable salt thereof is in a pharmaceutically acceptable carrier. 12. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol za uporabu prema zahtjevu 6, naznačen time što je rak HER2-negativan rak dojke ili karcinom pločastih stanica glave i vrata (SCCHN) kod subjekta.12. A compound according to claim 1, or a pharmaceutically acceptable salt thereof for use according to claim 6, characterized in that the cancer is HER2-negative breast cancer or squamous cell carcinoma of the head and neck (SCCHN) in the subject. 13. Spoj za uporabu prema bilo kojem od zahtjeva 5-10 i 12 naznačen time što je za uporabu u kombinaciji s terapijom zračenjem.13. A compound for use according to any one of claims 5-10 and 12, characterized in that it is for use in combination with radiation therapy. 14. Spoj za uporabu prema bilo kojem od zahtjeva 5-10 i 12-13 naznačen time što je za uporabu u kombinaciji s kirurškim zahvatom.14. A compound for use according to any one of claims 5-10 and 12-13 characterized in that it is for use in combination with a surgical procedure. 15. Spoj za uporabu prema bilo kojem od zahtjeva 5-10 i 12-14, naznačen time što je subjekt čovjek.15. A compound for use according to any one of claims 5-10 and 12-14, characterized in that the subject is human.
HRP20221385TT 2017-04-05 2018-04-03 Macrocyclic compound and uses thereof HRP20221385T1 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201762482030P 2017-04-05 2017-04-05
US201762526677P 2017-06-29 2017-06-29
US201762586416P 2017-11-15 2017-11-15
US15/814,105 US9938288B1 (en) 2017-04-05 2017-11-15 Macrocyclic compound and uses thereof
PCT/US2018/025887 WO2018187331A1 (en) 2017-04-05 2018-04-03 Macrocyclic compound and uses thereof
EP18719390.9A EP3606928B1 (en) 2017-04-05 2018-04-03 Macrocyclic compound and uses thereof

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US (2) US11725015B2 (en)
EP (2) EP3606928B1 (en)
JP (4) JP7168580B2 (en)
KR (2) KR102634732B1 (en)
CN (2) CN110831946B (en)
AU (2) AU2018250147B2 (en)
BR (1) BR112019020208A2 (en)
CA (1) CA3056945A1 (en)
CL (1) CL2019002854A1 (en)
CO (1) CO2019011538A2 (en)
DK (1) DK3606928T3 (en)
EC (1) ECSP19075677A (en)
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HR (1) HRP20221385T1 (en)
HU (1) HUE060466T2 (en)
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PH (1) PH12019502197A1 (en)
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PT (1) PT3606928T (en)
RS (1) RS63755B1 (en)
SA (1) SA519410259B1 (en)
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